ATE398125T1 - Chinazolin-derivate als tgf-beta-inhibitoren - Google Patents
Chinazolin-derivate als tgf-beta-inhibitorenInfo
- Publication number
- ATE398125T1 ATE398125T1 AT04718542T AT04718542T ATE398125T1 AT E398125 T1 ATE398125 T1 AT E398125T1 AT 04718542 T AT04718542 T AT 04718542T AT 04718542 T AT04718542 T AT 04718542T AT E398125 T1 ATE398125 T1 AT E398125T1
- Authority
- AT
- Austria
- Prior art keywords
- tgf beta
- quinazoline derivatives
- beta inhibitors
- mediated disease
- tgf
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 abstract 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 abstract 1
- 125000003258 trimethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])[*:1] 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45416403P | 2003-03-12 | 2003-03-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE398125T1 true ATE398125T1 (de) | 2008-07-15 |
Family
ID=32990876
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT04718542T ATE398125T1 (de) | 2003-03-12 | 2004-03-08 | Chinazolin-derivate als tgf-beta-inhibitoren |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7189733B2 (de) |
| EP (1) | EP1603908B1 (de) |
| AT (1) | ATE398125T1 (de) |
| DE (1) | DE602004014347D1 (de) |
| ES (1) | ES2305744T3 (de) |
| WO (1) | WO2004081009A1 (de) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030125344A1 (en) * | 2001-03-23 | 2003-07-03 | Bayer Corporation | Rho-kinase inhibitors |
| DE60218138T2 (de) * | 2001-03-23 | 2007-09-20 | Bayer Pharmaceuticals Corp., West Haven | Rho-kinase inhibitoren |
| CL2004000409A1 (es) * | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
| CA2520323C (en) * | 2003-04-09 | 2013-07-09 | Exelixis, Inc. | Tie-2 modulators and methods of use |
| US7718658B2 (en) * | 2004-09-02 | 2010-05-18 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US8283354B2 (en) * | 2004-09-02 | 2012-10-09 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| US7928107B2 (en) * | 2004-09-02 | 2011-04-19 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| MX2007007446A (es) * | 2004-12-17 | 2008-01-14 | Vertex Pharma | Procesos para la produccion de 4-aminoquinazolinas. |
| US7683066B2 (en) | 2005-05-20 | 2010-03-23 | Vertex Pharmaceuticals Incorporated | Isoquinolines useful as modulators of ion channels |
| KR101129868B1 (ko) | 2006-10-04 | 2012-04-12 | 화이자 프로덕츠 인코포레이티드 | 칼슘 수용체 길항제로서의 피리도[4,3-d]피리미딘-4(3H)-온 유도체 |
| AR070127A1 (es) * | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| WO2009146301A1 (en) * | 2008-05-27 | 2009-12-03 | Yale University | TARGETING TGF-β AS A THERAPY FOR ALZHEIMER'S DISEASE |
| EP2285380A4 (de) * | 2008-05-30 | 2012-03-14 | Summa Health Systems Llc | Verfahren zur verwendung von tgf-b-rezeptor-hemmern oder der aktivin-like-kinase (alk)-5-hemmer a-83-01 und sb-431542 zur behandlung von augenerkrankungen und wundheilungsleiden |
| US20100267731A1 (en) * | 2009-04-17 | 2010-10-21 | Summa Health Systems, LLC | Use of transforming growth factor-b receptor inhibitors to suppress ocular scarring |
| EA201200653A1 (ru) | 2009-11-07 | 2013-01-30 | Мерк Патент Гмбх | Гетариламинохинолины |
| EP2531500B1 (de) * | 2010-02-05 | 2018-01-24 | Merck Patent GmbH | Hetaryl-[1,8]naphthyridinderivate |
| TW201210597A (en) * | 2010-06-09 | 2012-03-16 | Gilead Sciences Inc | Inhibitors of hepatitis C virus |
| EA201300052A1 (ru) * | 2010-06-28 | 2013-06-28 | Мерк Патент Гмбх | [1,8]нафтиридиновые производные |
| KR20140022829A (ko) * | 2011-03-09 | 2014-02-25 | 메르크 파텐트 게엠베하 | 피리도 [2, 3 - b] 피라진 유도체 및 그 치료적 용도 |
| WO2014058317A1 (en) | 2012-10-10 | 2014-04-17 | Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis | Methods and means for predicting resistance to anti-cancer treatment |
| RS60371B1 (sr) | 2013-03-14 | 2020-07-31 | Brigham & Womens Hospital Inc | Sastavi i postupci za ekspanziju i kultivisanje epitelnih matičnih ćelija |
| KR101658111B1 (ko) * | 2013-05-13 | 2016-09-20 | 제일모직 주식회사 | 유기광전자소자용 화합물, 이를 포함하는 유기발광소자 및 상기 유기발광소자를 포함하는 표시장치 |
| CN103570632B (zh) * | 2013-07-22 | 2015-09-30 | 成都理工大学 | 无催化剂的4(3h)-喹唑啉酮的合成方法 |
| LT3089971T (lt) | 2014-01-01 | 2020-10-12 | Medivation Technologies Llc | Junginiai ir panaudojimo būdai |
| CA2959404A1 (en) | 2014-09-03 | 2016-03-10 | The Brigham And Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| EP3206689B1 (de) | 2014-10-14 | 2021-12-08 | La Jolla Institute of Allergy & Immunology | Inhibitoren von niedermolekularer protein-tyrosinphosphatase und verwendungen davon |
| EP3313420B1 (de) | 2015-06-25 | 2024-03-13 | The Children's Medical Center Corporation | Verfahren und zusammensetzungen in bezug auf hämatopoetische stammzellenexpansion, -anreicherung und -pflege |
| CN108137597A (zh) * | 2015-07-28 | 2018-06-08 | 百时美施贵宝公司 | TGFβ受体拮抗剂 |
| JP2019506153A (ja) | 2016-01-08 | 2019-03-07 | マサチューセッツ インスティテュート オブ テクノロジー | 分化した腸内分泌細胞およびインスリン産生細胞の作製 |
| US11583593B2 (en) | 2016-01-14 | 2023-02-21 | Synthis Therapeutics, Inc. | Antibody-ALK5 inhibitor conjugates and their uses |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| US20190119642A1 (en) | 2016-03-15 | 2019-04-25 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| WO2018125746A1 (en) | 2016-12-30 | 2018-07-05 | Frequency Therapeutics, Inc. | 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| US11066420B2 (en) | 2017-05-01 | 2021-07-20 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitors of low molecular weight protein tyrosine phosphatase (LMPTP) and uses thereof |
| CN109096254B (zh) * | 2017-06-20 | 2021-07-06 | 江西师范大学 | 喹唑啉衍生物及其制备方法和应用 |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| US20210254006A1 (en) | 2018-06-06 | 2021-08-19 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| CN113195707A (zh) | 2018-08-17 | 2021-07-30 | 频率治疗公司 | 用于通过上调jag-1来生成毛细胞的组合物和方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| AU2019419414A1 (en) | 2018-12-31 | 2023-04-06 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| EP4313967B1 (de) | 2021-03-29 | 2025-11-12 | Gilead Sciences, Inc. | Khk-hemmer |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5776963A (en) * | 1989-05-19 | 1998-07-07 | Hoechst Marion Roussel, Inc. | 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility |
| US5223501A (en) * | 1991-05-10 | 1993-06-29 | Merck & Co., Inc. | Substituted pyrimidinones bearing acidic functional groups as angiotensin ii antagonists |
| US6225318B1 (en) * | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
| US6184226B1 (en) | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| US20040038856A1 (en) | 2002-05-17 | 2004-02-26 | Sarvajit Chakravarty | Treatment of fibroproliferative disorders using TGF-beta inhibitors |
| CA2494367A1 (en) | 2002-07-25 | 2004-02-05 | Scios Inc. | Methods for improvement of lung function using tgf-.beta. inhibitors |
-
2004
- 2004-03-08 AT AT04718542T patent/ATE398125T1/de not_active IP Right Cessation
- 2004-03-08 WO PCT/US2004/007090 patent/WO2004081009A1/en not_active Ceased
- 2004-03-08 DE DE602004014347T patent/DE602004014347D1/de not_active Expired - Lifetime
- 2004-03-08 EP EP04718542A patent/EP1603908B1/de not_active Expired - Lifetime
- 2004-03-08 ES ES04718542T patent/ES2305744T3/es not_active Expired - Lifetime
- 2004-03-08 US US10/795,538 patent/US7189733B2/en not_active Expired - Fee Related
-
2007
- 2007-01-16 US US11/653,679 patent/US8268857B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE602004014347D1 (de) | 2008-07-24 |
| ES2305744T3 (es) | 2008-11-01 |
| US7189733B2 (en) | 2007-03-13 |
| US8268857B2 (en) | 2012-09-18 |
| EP1603908A1 (de) | 2005-12-14 |
| WO2004081009A1 (en) | 2004-09-23 |
| US20070142408A1 (en) | 2007-06-21 |
| US20040204431A1 (en) | 2004-10-14 |
| EP1603908B1 (de) | 2008-06-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |